RU2016121410A - A NEW DERIVATIVE OF 3-AZABICYCLO [3.1.0] HEXAN AND ITS APPLICATION FOR MEDICAL PURPOSES - Google Patents

A NEW DERIVATIVE OF 3-AZABICYCLO [3.1.0] HEXAN AND ITS APPLICATION FOR MEDICAL PURPOSES Download PDF

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RU2016121410A
RU2016121410A RU2016121410A RU2016121410A RU2016121410A RU 2016121410 A RU2016121410 A RU 2016121410A RU 2016121410 A RU2016121410 A RU 2016121410A RU 2016121410 A RU2016121410 A RU 2016121410A RU 2016121410 A RU2016121410 A RU 2016121410A
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hexan
azabicyclo
ethyl
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cyclopropanesulfonamide
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RU2701861C1 (en
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Каори ТАНИКО
Тосиюки МИЯДЗАВА
Тацурох КАНЕКО
Дайсуке КУРУМАДЗУКА
Сатоко ХАРАДА
Тору ИДЗУТИ
Морио ОКАБЕ
Рио Ивамура
Ясунори ЦУДЗАКИ
Хироюки СЕТОГУТИ
Юуки ИМУРА
Хирото АКАДЗА
Мотохиса СИМИДЗУ
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Санва Кагаку Кенкюсо Ко., Лтд.
Убе Индастриз, Лтд.
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
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    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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Claims (50)

1. Соединение, представленное общей формулой (I), или его фармакологически приемлемая соль:1. The compound represented by General formula (I), or its pharmacologically acceptable salt:
Figure 00000001
,
Figure 00000001
, в которой R1 и R2 являются одинаковыми или различными, и каждый представляет собой атом водорода или атом галогена, при условии, что R1 и R2 не являются одновременно атомами галогена,in which R 1 and R 2 are the same or different, and each represents a hydrogen atom or a halogen atom, provided that R 1 and R 2 are not simultaneously halogen atoms, R3 представляет собой C1-C3 алкильную группу или винильную группу, иR 3 represents a C 1 -C 3 alkyl group or a vinyl group, and R4 соответствует формуле (II):R 4 corresponds to the formula (II):
Figure 00000002
,
Figure 00000002
, в которой R5 представляет собой гидрокси группу или C1-C3 алкокси группу, и R6 и R7 являются одинаковыми или различными, и каждый представляет собой атом водорода или атом галогена;in which R 5 represents a hydroxy group or a C 1 -C 3 alkoxy group, and R 6 and R 7 are the same or different, and each represents a hydrogen atom or a halogen atom; или формула (III):or formula (III):
Figure 00000003
,
Figure 00000003
, в которой кольцо A представляет собой замещенную атомом(ами) галогена C5-C7 циклоалкильную группу, которая необязательно замещена C1-C3 алкокси группой, или замещенную атомом(ами) галогена 5-7-членную насыщенную гетероциклическую группу.in which ring A represents a C 5 -C 7 halogen atom (s) substituted by a cycloalkyl group, which is optionally substituted by a C 1 -C 3 alkoxy group, or a 5-7 membered saturated heterocyclic group substituted by a halogen atom (s). 2. Соединение или его фармакологически приемлемая соль по п.1, где R1 представляет собой атом водорода в общей формуле (I).2. The compound or its pharmacologically acceptable salt according to claim 1, where R 1 represents a hydrogen atom in the General formula (I). 3. Соединение или его фармакологически приемлемая соль по п.1, где R3 представляет собой метильную группу, этильную группу или винильную группу в общей формуле (I).3. The compound or its pharmacologically acceptable salt according to claim 1, where R 3 represents a methyl group, an ethyl group or a vinyl group in the General formula (I). 4. Соединение или его фармакологически приемлемая соль по п.1, где R4 соответствует формуле (II) в общей формуле (I):4. The compound or its pharmacologically acceptable salt according to claim 1, where R 4 corresponds to the formula (II) in the general formula (I):
Figure 00000004
,
Figure 00000004
, в которой R5 представляет собой гидрокси группу или C1-C3 алкокси группу, и R6 и R7 являются одинаковыми или различными, и каждый представляет собой атом водорода или атом галогена.in which R 5 represents a hydroxy group or a C 1 -C 3 alkoxy group, and R 6 and R 7 are the same or different, and each represents a hydrogen atom or a halogen atom. 5. Соединение или его фармакологически приемлемая соль по п.4, где R5 представляет собой гидрокси группу или метокси группу, и R6 и R7, каждый, представляют собой атом водорода в формуле (II).5. The compound or its pharmacologically acceptable salt according to claim 4, where R 5 represents a hydroxy group or a methoxy group, and R 6 and R 7 each represent a hydrogen atom in the formula (II). 6. Соединение или его фармакологически приемлемая соль по п.5, где R1 представляет собой атом водорода, R2 представляет собой атом водорода или атом фтора, и R3 представляет собой этильную группу в общей формуле (I).6. The compound or its pharmacologically acceptable salt according to claim 5, where R 1 represents a hydrogen atom, R 2 represents a hydrogen atom or a fluorine atom, and R 3 represents an ethyl group in the General formula (I). 7. Соединение или его фармакологически приемлемая соль по п.1, где R4 соответствует формуле (III):7. The compound or its pharmacologically acceptable salt according to claim 1, where R 4 corresponds to the formula (III):
Figure 00000005
,
Figure 00000005
, в которой кольцо A представляет собой замещенную атомом(ами) галогена C5-C7 циклоалкильную группу, которая необязательно замещена C1-C3 алкокси группой, или замещенную атомом(ами) галогена 5-7-членную насыщенную гетероциклическую группу в общей формуле (I).in which ring A represents a substituted C 5 -C 7 halogen atom (s) by a cycloalkyl group, which is optionally substituted by a C 1 -C 3 alkoxy group, or a 5-7 membered saturated heterocyclic group substituted by a halogen atom (s) in the general formula ( I). 8. Соединение или его фармакологически приемлемая соль по п.7, где кольцо A представляет собой замещенную атомом(ами) хлора циклогексильную группу, которая необязательно замещена C1-C3 алкокси группой, или замещенную атомом(ами) фтора 5-6-членную азотсодержащую насыщенную гетероциклическую группу в формуле (III).8. The compound or its pharmacologically acceptable salt according to claim 7, where ring A represents a substituted by a chlorine atom (s) cyclohexyl group, which is optionally substituted by a C 1 -C 3 alkoxy group, or substituted by a 5-6-membered fluorine atom (s) a nitrogen-containing saturated heterocyclic group in the formula (III). 9. Соединение или его фармакологически приемлемая соль по п.8, где кольцо A представляет собой любую группу, выбранную из следующей группы:9. The compound or its pharmacologically acceptable salt of claim 8, where ring A represents any group selected from the following group:
Figure 00000006
Figure 00000006
 в формуле (III).in the formula (III). 10. Соединение или его фармакологически приемлемая соль по п.8, где R1 представляет собой атом водорода, R2 представляет собой атом водорода или атом фтора, и R3 представляет собой этильную группу в общей формуле (I).10. The compound or its pharmacologically acceptable salt of claim 8, where R 1 represents a hydrogen atom, R 2 represents a hydrogen atom or a fluorine atom, and R 3 represents an ethyl group in the General formula (I). 11. Соединение или его фармакологически приемлемая соль по п.9, где R1 представляет собой атом водорода, R2 представляет собой атом водорода или атом фтора, и R3 представляет собой этильную группу в общей формуле (I).11. The compound or its pharmacologically acceptable salt according to claim 9, where R 1 represents a hydrogen atom, R 2 represents a hydrogen atom or a fluorine atom, and R 3 represents an ethyl group in the general formula (I). 12. Соединение или его фармакологически приемлемая соль по п.4, которое выбрано из группы, состоящей из:12. The compound or its pharmacologically acceptable salt according to claim 4, which is selected from the group consisting of: N-(3-{(1R,5S,6r)-6-этил-3-[(2-гидрокси-2,3-дигидро-1H-инден-2-ил)метил]-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -6-ethyl-3 - [(2-hydroxy-2,3-dihydro-1H-inden-2-yl) methyl] -3-azabicyclo [3.1.0 ] hexan-6-yl} phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-6-этил-3-[(2-гидрокси-2,3-дигидро-1H-инден-2-ил)метил]-3-азабицикло[3.1.0]гексан-6-ил}-4-фторфенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -6-ethyl-3 - [(2-hydroxy-2,3-dihydro-1H-inden-2-yl) methyl] -3-azabicyclo [3.1.0 ] hexan-6-yl} -4-fluorophenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-6-этил-3-[(2-метокси-2,3-дигидро-1H-инден-2-ил)метил]-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -6-ethyl-3 - [(2-methoxy-2,3-dihydro-1H-inden-2-yl) methyl] -3-azabicyclo [3.1.0 ] hexan-6-yl} phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-6-этил-3-[(2-гидрокси-2,3-дигидро-1H-инден-2-ил)метил]-3-азабицикло[3.1.0]гексан-6-ил}-5-фторфенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -6-ethyl-3 - [(2-hydroxy-2,3-dihydro-1H-inden-2-yl) methyl] -3-azabicyclo [3.1.0 ] hexan-6-yl} -5-fluorophenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-6-этил-3-[(2-метокси-2,3-дигидро-1H-инден-2-ил)метил]-3-азабицикло[3.1.0]гексан-6-ил}-4-фторфенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -6-ethyl-3 - [(2-methoxy-2,3-dihydro-1H-inden-2-yl) methyl] -3-azabicyclo [3.1.0 ] hexan-6-yl} -4-fluorophenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-6-этил-3-[(2-метокси-2,3-дигидро-1H-инден-2-ил)метил]-3-азабицикло[3.1.0]гексан-6-ил}-5-фторфенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -6-ethyl-3 - [(2-methoxy-2,3-dihydro-1H-inden-2-yl) methyl] -3-azabicyclo [3.1.0 ] hexan-6-yl} -5-fluorophenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[(2-этокси-2,3-дигидро-1H-инден-2-ил)метил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3 - [(2-ethoxy-2,3-dihydro-1H-inden-2-yl) methyl] -6-ethyl-3-azabicyclo [3.1.0 ] hexan-6-yl} phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[(2-гидрокси-2,3-дигидро-1H-инден-2-ил)метил]-6-метил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3 - [(2-hydroxy-2,3-dihydro-1H-inden-2-yl) methyl] -6-methyl-3-azabicyclo [3.1.0 ] hexan-6-yl} phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[(2-метокси-2,3-дигидро-1H-инден-2-ил)метил]-6-метил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3 - [(2-methoxy-2,3-dihydro-1H-inden-2-yl) methyl] -6-methyl-3-azabicyclo [3.1.0 ] hexan-6-yl} phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[(2-гидрокси-2,3-дигидро-1H-инден-2-ил)метил]-6-винил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида иN- (3 - {(1R, 5S, 6r) -3 - [(2-hydroxy-2,3-dihydro-1H-inden-2-yl) methyl] -6-vinyl-3-azabicyclo [3.1.0 ] hexan-6-yl} phenyl) cyclopropanesulfonamide and N-(3-{(1R,5S,6r)-3-[(5,6-дифтор-2-гидрокси-2,3-дигидро-1H-инден-2-ил)метил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида.N- (3 - {(1R, 5S, 6r) -3 - [(5,6-difluoro-2-hydroxy-2,3-dihydro-1H-inden-2-yl) methyl] -6-ethyl-3 -azabicyclo [3.1.0] hexan-6-yl} phenyl) cyclopropanesulfonamide. 13. Соединение или его фармакологически приемлемая соль по п.7, которое выбрано из группы, состоящей из:13. The compound or its pharmacologically acceptable salt according to claim 7, which is selected from the group consisting of: N-(3-{(1R,5S,6r)-3-[3-(4,4-дифторциклогексил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3- [3- (4,4-difluorocyclohexyl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl} phenyl) cyclopropanesulfonamide , N-(3-{(1R,5S,6r)-3-[3-(4,4-дифторциклогексил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}-4-фторфенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3- [3- (4,4-difluorocyclohexyl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl} -4- fluorophenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[3-(4,4-дифтор-1-метоксициклогексил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3- [3- (4,4-difluoro-1-methoxycyclohexyl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl } phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[3-(4,4-дифторпиперидин-1-ил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3- [3- (4,4-difluoropiperidin-1-yl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl } phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[3-(3,3-дифторпирролидин-1-ил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3- [3- (3,3-difluoropyrrolidin-1-yl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl } phenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[3-(3,3-дифторпирролидин-1-ил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}-4-фторфенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3- [3- (3,3-difluoropyrrolidin-1-yl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl } -4-fluorophenyl) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[1-этокси-(4,4-дифторциклогексил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида,N- (3 - {(1R, 5S, 6r) -3- [1-ethoxy- (4,4-difluorocyclohexyl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl} phenyl ) cyclopropanesulfonamide, N-(3-{(1R,5S,6r)-3-[3-(4,4-дифторпиперидин-1-ил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}-4-фторфенил)циклопропансульфонамида иN- (3 - {(1R, 5S, 6r) -3- [3- (4,4-difluoropiperidin-1-yl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl } -4-fluorophenyl) cyclopropanesulfonamide and N-(3-{(1R,5S,6r)-3-[3-(3,3-дифторпиперидин-1-ил)пропил]-6-этил-3-азабицикло[3.1.0]гексан-6-ил}фенил)циклопропансульфонамида.N- (3 - {(1R, 5S, 6r) -3- [3- (3,3-difluoropiperidin-1-yl) propyl] -6-ethyl-3-azabicyclo [3.1.0] hexan-6-yl } phenyl) cyclopropanesulfonamide. 14. Лекарственное средство, содержащее соединение или его фармакологически приемлемую соль по любому из пп.1-13 в качестве активного ингредиента.14. A medicament containing the compound or its pharmacologically acceptable salt according to any one of claims 1 to 13 as an active ingredient. 15. Лекарственное средство по п.14 для применения в профилактике или лечении зуда. 15. The drug according to 14 for use in the prevention or treatment of pruritus.
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